The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio- and esterderivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-30,40- dithioglycol (1) and avarol-40-(3)mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 mg and IC50 0.05mM and 0.50 mg and IC50 0.12 mM, respectively), while 40-tryptamine-avarone (9) and avarol-30-(3)mercaptopropionic acid (2) exhibited the highest cytotoxicity against the human breast T-47D cancer cell line (IC50 0.66 mg/ mL and 1.25 mg/mL, respectively). According to experimental data obtained, the sesquiterpenoid hydroquinone structure of bioactive avarol derivatives may inspire development of new pharmacologically useful substances to be used in the treatment of Alzheimer's disease and/or human breast tumour.
Further in vitro biological activity evaluation of amino-, thio- and ester- derivatives of avarol
Tommonaro G;Iodice C;
2014
Abstract
The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio- and esterderivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-30,40- dithioglycol (1) and avarol-40-(3)mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 mg and IC50 0.05mM and 0.50 mg and IC50 0.12 mM, respectively), while 40-tryptamine-avarone (9) and avarol-30-(3)mercaptopropionic acid (2) exhibited the highest cytotoxicity against the human breast T-47D cancer cell line (IC50 0.66 mg/ mL and 1.25 mg/mL, respectively). According to experimental data obtained, the sesquiterpenoid hydroquinone structure of bioactive avarol derivatives may inspire development of new pharmacologically useful substances to be used in the treatment of Alzheimer's disease and/or human breast tumour.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
